Forodesine hydrochloride BCX-1777 hydrochloride; Immucillin-H hydrochloride|cas:284490-13-7|西域试剂

Forodesine hydrochloride BCX-1777 hydrochloride; Immucillin-H hydrochloride,99.34%

产品编号：Bellancom-16209| CAS NO：284490-13-7| 分子式：C₁₁H₁₅ClN₄O₄| 分子量：302.71

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货号	价格	库存与货期
Bellancom-16209	￥550.00	杭州北京（现货）
Bellancom-16209	￥1200.00	杭州北京（现货）
Bellancom-16209	￥1800.00	杭州北京（现货）
Bellancom-16209	￥2800.00	杭州北京（现货）
Bellancom-16209	￥5100.00	杭州北京（现货）

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Forodesine hydrochloride BCX-1777 hydrochloride; Immucillin-H hydrochloride

产品介绍

Forodesine hydrochloride (BCX-1777 hydrochloride) 是一种高效的口服活性的嘌呤核苷磷酸化酶 (PNP) 抑制剂，对人，小鼠，大鼠，猴和狗 PNP 的 IC₅₀ 值在 0.48 至 1.57 nM 之间。Forodesine hydrochloride 是有效的人类淋巴细胞增殖抑制剂，可通过增加 dGTP 水平而诱导白血病细胞凋亡 (apoptosis)。

生物活性

Forodesine hydrochloride (BCX-1777 hydrochloride) is a highly potent and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC₅₀ values ranging from 0.48 to 1.57 nM for human, mouse, rat, monkey and dog PNP. Forodesine hydrochloride is a potent human lymphocyte proliferation inhibitor. Forodesine hydrochloride could induce apoptosis in leukemic cells by increasing the dGTP levels.

体外研究

Forodesine (10-30 μM; 24 and 48 hours; RPMI-8226, MOLT-4 and 5T33MM cells) treatment is partially inhibition of proliferation.
Forodesine (10-30 μM; 24 and 48 hours; RPMI-8226, MOLT-4 and 5T33MM cells) has no effect on the MM cells at 24 hours, while it could reduce the percentage of living cells in the MOLT-4 cells with 40%.
Forodesine (BCX-1777), in the presence of 2'-deoxyguanosine (dGuo, 3-10 μM), inhibits human lymphocyte proliferation activated by various agents such as interleukin-2 (IL-2), mixed lymphocyte reaction (MLR) and phytohemagglutinin (PHA) (IC₅₀ values < 0.1-0.38 μM).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line:	Human RPMI-8226, human MOLT-4 (T-ALL) cells, 5T33MM (Multiple myeloma, MM).
Concentration:	10 μM, 20 μM, 30 μM
Incubation Time:	24 and 48 hours
Result:	At the effects at 48 hours, a complete block in proliferation in the MOLT-4 cells and 15% reduction in the 5T33MM cells.

Apoptosis Analysis

Cell Line:	Human RPMI-8226, human MOLT-4 (T-ALL) cells, 5T33MM (Multiple myeloma, MM).
Concentration:	10 μM, 20 μM, 30 μM
Incubation Time:	24 and 48 hours
Result:	A limited induction of apoptosis.

体内研究
(In Vivo)

Forodesine (BCX-1777) has excellent oral bioavailability (63%) in mice.
At a single dose of 10 mg/kg in mice, Forodesine elevates dGuo to approximately 5 μM.
n the human peripheral blood lymphocyte severe combined immunodeficiency (hu-PBL-SCID) mouse model, Forodesine is effective in prolonging the life span 2-fold or more.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

H₂O : 100 mg/mL (330.35 mM; Need ultrasonic)

DMSO : 10 mg/mL (33.03 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.3035 mL	16.5175 mL	33.0349 mL
5 mM	0.6607 mL	3.3035 mL	6.6070 mL
10 mM	0.3303 mL	1.6517 mL	3.3035 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： PBS
Solubility: 36.67 mg/mL (121.14 mM); Clear solution; Need ultrasonic
2.

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: ≥ 0.5 mg/mL (1.65 mM); Clear solution
3.

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 0.5 mg/mL (1.65 mM); Clear solution